(+)-JQ1

目录号：S7110 Purity: 99.99%

(+)-JQ1是一种BET bromodomain抑制剂，作用于BRD4(1/2)，无细胞试验中IC50为77 nM/33 nM，结合到BET家族的所有溴结构域，而不结合到BET家族以外的溴结构域。(+)-JQ1可通过诱导自噬来抑制细胞增殖。(+)-JQ1 可抑制 Nuclear receptor binding SET domain protein 3 (NSD3) 的靶基因表达。

(+)-JQ1 Chemical Structure

CAS: 1268524-70-4

规格	价格	库存
10mM (1mL in DMSO)	794.43	现货
10mg	1040.13	现货
25mg	1941.03	现货
100mg	4823.91	现货
1g	7944.3	现货
更大包装有超大折扣
400-668-6834 info@selleck.cn

产品质控

批次：纯度： 99.99%

99.99

(+)-JQ1相关产品

相关产品	Quizartinib (AC220)	点击展开
相关化合物库	激酶抑制剂库 FDA药物库天然产物库已知活性药物库-I 生物活性库Ⅱ	点击展开

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
ROSA KIT D816V	Apoptosis Assay	200-5000 nM	48 h	induces cell apoptosis in a dose-dependent manner	26055303
ROSA KIT WT	Apoptosis Assay	200-5000 nM	48 h	induces cell apoptosis in a dose-dependent manner	26055303
HMC-1.2	Apoptosis Assay	200-5000 nM	48 h	induces cell apoptosis in a dose-dependent manner	26055303
HMC-1.1	Apoptosis Assay	200-5000 nM	48 h	induces cell apoptosis in a dose-dependent manner	26055303
ROSA KIT D816V	Growth Inhibition Assay	5-5000 nM	48 h	inhibits cell growth in a dose-dependent manner	26055303
ROSA KIT WT	Growth Inhibition Assay	5-5000 nM	48 h	inhibits cell growth in a dose-dependent manner	26055303
HMC-1.2	Growth Inhibition Assay	5-5000 nM	48 h	inhibits cell growth in a dose-dependent manner	26055303
HMC-1.1	Growth Inhibition Assay	5-5000 nM	48 h	inhibits cell growth in a dose-dependent manner	26055303
SK-N-DZ	Cell Viability Assay	1 μM	1-4 d	decreases cell viability significantly	26067464
SK-N-SH	Cell Viability Assay	1 μM	1-4 d	decreases cell viability significantly	26067464
BE(2)-M17	Cell Viability Assay	1 μM	1-4 d	decreases cell viability significantly	26067464
JF	Cell Viability Assay	1 μM	1-4 d	decreases cell viability significantly	26067464
IMR-32	Cell Viability Assay	1 μM	1-4 d	decreases cell viability significantly	26067464
BE(2)-C	Cell Viability Assay	1 μM	1-4 d	decreases cell viability significantly	26067464
DDR2L63V	Cell Viability Assay	0-1 μM	5 d	decreases cell viability in a dose-dependent manner	26206333
858	Cell Viability Assay	0-1 μM	5 d	decreases cell viability in a dose-dependent manner	26206333
HEK293	Function Assay	100/400/1000 nM	24 h	upregulates and activates SIRT1	26212199
MCF-7	Function Assay	100/400/1000 nM	24 h	upregulates and activates SIRT1	26212199
A549	Function Assay	100/400/1000 nM	24 h	upregulates and activates SIRT1	26212199
Omm1.3	Cell Cycle Assay	500 nM	24/48/72 h	induces the cell accumulation at sub-G1	26397223
92.1	Cell Cycle Assay	500 nM	24/48/72 h	induces the cell accumulation at sub-G1	26397223
Omm1.3	Apoptosis Assay	500 nM	48 h	induces apoptosis	26397223
92.1	Apoptosis Assay	500 nM	48 h	induces apoptosis	26397223
Omm1	Cell Viability Assay	0-2 μM	4 d	decreases cell viability in a dose-dependent manner	26397223
Mel270	Cell Viability Assay	0-2 μM	4 d	decreases cell viability in a dose-dependent manner	26397223
Mel202	Cell Viability Assay	0-2 μM	4 d	decreases cell viability in a dose-dependent manner	26397223
Omm1.3	Cell Viability Assay	0-2 μM	4 d	decreases cell viability in a dose-dependent manner	26397223
92.1	Cell Viability Assay	0-2 μM	4 d	decreases cell viability in a dose-dependent manner	26397223
Mel290	Cell Viability Assay	0-2 μM	4 d	decreases cell viability in a dose-dependent manner	26397223
Mel285	Cell Viability Assay	0-2 μM	4 d	decreases cell viability in a dose-dependent manner	26397223
C8161	Cell Viability Assay	0-2 μM	4 d	decreases cell viability in a dose-dependent manner	26397223
H1299	Function Assay	1/2.5/5 μM	12 h	decreased DR4 expression	26415225
H157	Function Assay	1/2.5/5 μM	12 h	decreased DR4 expression	26415225
H1299	Function Assay	1/2.5/5 μM	12 h	weakly decreased Bcl-2 levels	26415225
A549	Function Assay	1/2.5/5 μM	12 h	weakly decreased Bcl-2 levels	26415225
H1299	Growth Inhibition Assay	0.1-10 μM	72 h	inhibits cell growth in a dose-dependent manner	26415225
H157	Growth Inhibition Assay	0.1-10 μM	72 h	inhibits cell growth in a dose-dependent manner	26415225
A549	Growth Inhibition Assay	0.1-10 μM	72 h	inhibits cell growth in a dose-dependent manner	26415225
HCCLM3	Apoptosis Assay	0.1/0.5/2.5 μM	48 h	activates caspase-3 and caspase-9 expression and induced PARP cleavage as well as cytochrome c release into the cytoplasm from mitochondria	26575167
Hep3B	Apoptosis Assay	0.1/0.5/2.5 μM	48 h	activates caspase-3 and caspase-9 expression and induced PARP cleavage as well as cytochrome c release into the cytoplasm from mitochondria	26575167
HCCLM3	Cell Cycle Assay	0.1/0.5/2.5 μM	48 h	leads to a substantial accumulation of HCC cells in sub-G1 phase	26575167
Hep3B	Cell Cycle Assay	0.1/0.5/2.5 μM	48 h	leads to a substantial accumulation of HCC cells in sub-G1 phase	26575167
MHCC97H	Growth Inhibition Assay	0-10 μM	5 d	IC50=0.41 μM	26575167
BEL7402	Growth Inhibition Assay	0-10 μM	5 d	IC50=0.47 μM	26575167
SMMC7721	Growth Inhibition Assay	0-10 μM	5 d	IC50=0.41 μM	26575167
HepG2	Growth Inhibition Assay	0-10 μM	5 d	IC50=0.34 μM	26575167
HuH7	Growth Inhibition Assay	0-10 μM	5 d	IC50=0.21 μM	26575167
HCCLM3	Growth Inhibition Assay	0-10 μM	5 d	IC50=0.14 μM	26575167
Hep3B	Growth Inhibition Assay	0-10 μM	5 d	IC50=0.08 μM	26575167
BCPAP	Cell Cycle Assay	250/500/1000 nM	72 h	arrests cell cycle at G0/G1 phase	26707881
K1	Cell Cycle Assay	250/500/1000 nM	72 h	arrests cell cycle at G0/G1 phase	26707881
BCPAP	Cell Viability Assay	250/500/1000 nM	24/48/72 h	inhibits cell viability in both dose- and time- dependent manner	26707881
K1	Cell Viability Assay	250/500/1000 nM	24/48/72 h	inhibits cell viability in both dose- and time- dependent manner	26707881
494H	Apoptosis Assay	0.25/0.5/1.0 μM	24 h	increases levels of cleaved caspase-3	25944566
148I	Apoptosis Assay	0.25/0.5/1.0 μM	24 h	increases levels of cleaved caspase-3	25944566
OS17	Apoptosis Assay	0.25/0.5/1.0 μM	24 h	increases levels of cleaved caspase-3	25944566
494H	Apoptosis Assay	1 μM	48 h	induces cell apoptosis significantly	25944566
148I	Apoptosis Assay	1 μM	48 h	induces cell apoptosis significantly	25944566
OS17	Apoptosis Assay	1 μM	48 h	induces cell apoptosis significantly	25944566
MOLM13	Apoptosis Assay	250 nM	48 h	induces significantly apoptosis cotreatment with quizartinib	25053825
MV4-11	Apoptosis Assay	250 nM	48 h	induces significantly apoptosis cotreatment with quizartinib	25053825
MOLM13	Function Assay	250 nM	24 h	enhances quizartinib-induced more p21, BIM, and cleaved PARP	25053825
MV4-11	Function Assay	250 nM	24 h	enhances quizartinib-induced more p21, BIM, and cleaved PARP	25053825
MOLM13	Apoptosis Assay	250 nM	48 h	induces significantly apoptosis cotreatment with ponatinib	25053825
MV4-11	Apoptosis Assay	250 nM	48 h	induces significantly apoptosis cotreatment with ponatinib	25053825
Hela	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
HBL-1	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
HLY-1	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
OCI-Ly3	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
OCI-Ly10	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
SU-DHL-4	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
SU-DHL-5	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
SU-DHL-6	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
SU-DHL-10	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
RC-K8	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
OCI-Ly8	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
OCL-Ly18	Cell Viability Assay	0-500 nM	72 h	decreases cell viability in a dose-dependent manner	25009295
OCI-Ly3	Growth Inhibition Assay	172/250/500 nM	2/7 d	induces cell-cycle arrest at sub-G1 with minimal cell death	25009295
OCI-Ly8	Growth Inhibition Assay	172/250/500 nM	2/7 d	induces cell-cycle arrest at sub-G1 with minimal cell death	25009295
SU-DHL-4	Growth Inhibition Assay	172/250/500 nM	2/7 d	induces cell-cycle arrest at sub-G1 with minimal cell death	25009295
SU-DHL-10	Growth Inhibition Assay	172/250/500 nM	2/7 d	induces cell-cycle arrest at sub-G1 with minimal cell death	25009295
OCI-Ly3	Apoptosis Assay	172/250 nM	7d	increases caspase-3/7 activity significantly	25009295
OCI-Ly8	Apoptosis Assay	172/250 nM	7d	increases caspase-3/7 activity significantly	25009295
SU-DHL-4	Apoptosis Assay	172/250 nM	7d	increases caspase-3/7 activity significantly	25009295
SU-DHL-10	Apoptosis Assay	172/250 nM	7d	increases caspase-3/7 activity significantly	25009295
494L	Growth Inhibition Assay		72 h	IC50=0.317±0.012 μM	25944566
89R	Growth Inhibition Assay		72 h	IC50=0.126±0.003 μM	25944566
98Sc	Growth Inhibition Assay		72 h	IC50=0.115±0.004 μM	25944566
148I	Growth Inhibition Assay		72 h	IC50=0.284±0.035 μM	25944566
716H	Growth Inhibition Assay		72 h	IC50=0.212±0.034 μM	25944566
493H	Growth Inhibition Assay		72 h	IC50=0.047±0.009 μM	25944566
494H	Growth Inhibition Assay		72 h	IC50=0.122±0.004 μM	25944566
493L	Growth Inhibition Assay		72 h	IC50=0.050±0.011 μM	25944566
148L	Growth Inhibition Assay		72 h	IC50=0.146±0.017 μM	25944566
98L	Growth Inhibition Assay		72 h	IC50=0.309±0.029 μM	25944566
OS17	Growth Inhibition Assay		72 h	IC50=0.079±0.003 μM	25944566
OS9	Growth Inhibition Assay		72 h	IC50=0.406±0.028 μM	25944566
MG63	Growth Inhibition Assay		72 h	IC50=0.114±0.025 μM	25944566
SAOS2	Growth Inhibition Assay		72 h	IC50=0.217±0.003 μM	25944566
U2OS	Growth Inhibition Assay		72 h	IC50=0.198±0.008 μM	25944566
SJSA-1	Growth Inhibition Assay		72 h	IC50=0.100±0.010 μM	25944566
Rosetta2 DE3	Fluorescence polarization assay		30 mins	Ki = 0.0066 μM	26080064
Rosetta2 DE3	Fluorescence polarization assay		30 mins	Ki = 0.0076 μM	26080064
Rosetta2 DE3	Fluorescence polarization assay		30 mins	Ki = 0.0089 μM	26080064
Rosetta2 DE3	Fluorescence polarization assay		30 mins	Ki = 0.0107 μM	26080064
MV4-11	Antiproliferative activity assay		72 h	IC50 = 0.012 μM	26731490
Rosetta2 DE3	Fluorescence polarization assay		30 mins	Ki = 0.012 μM	29758518
VCaP	Antiproliferative activity assay		12 h	IC50 = 0.012 μM	28463487
Rosetta2 DE3	Fluorescence polarization assay		30 mins	Ki = 0.0125 μM	26080064
Rosetta2 DE3	Fluorescence polarization assay		30 mins	Ki = 0.0132 μM	26080064
Rosetta2 DE3	Fluorescence polarization assay		30 mins	Ki = 0.0149 μM	28463487
TY82	Antiproliferative activity assay		72 h	IC50 = 0.018 μM	28586718
MM1S	Antiproliferative activity assay		72 h	IC50 = 0.019 μM	28586718
MM1S	Cytotoxicity assay		72 h	IC50 = 0.02 μM	29758518
HT-29	Antiproliferative activity assay		12 h	IC50 = 0.02 μM	28535045
MV4-11	Growth inhibition assay		72 h	IC50 = 0.023 μM	25559428
MV4-11	Cytotoxicity assay		4 days	IC50 = 0.024 μM	28463487
MV4-11	Growth inhibition assay		4 days	IC50 = 0.024 μM	26080064
Rosetta2 DE3	Function assay		30 mins	IC50 = 0.0287 μM	26080064
NALM16	Cytotoxicity assay		5 days	EC50 = 0.03 μM	29170024
BL21(DE3)-R3-pRARE2	Function assay		30 mins	IC50 = 0.033 μM	28195723
Rosetta2 DE3	Fluorescence polarization assay		30 mins	IC50 = 0.0357 μM	26080064
Rosetta2 DE3	Fluorescence polarization assay		30 mins	IC50 = 0.0422 μM	28463487
Rosetta2 DE3	Fluorescence polarization assay		30 mins	IC50 = 0.0467 μM	28463487
MOLM13	Cytotoxicity assay		4 days	IC50 = 0.056 μM	28463487
MOLM13	Growth inhibition assay		4 days	IC50 = 0.056 μM	26080064
HL60	Antiproliferative activity assay		72 h	IC50 = 0.06 μM	29170024
HL60	Growth inhibition assay		3 days	GC50 = 0.06 μM	29657099
NALM6	Cytotoxicity assay		5 days	EC50 = 0.06 μM	28549889
Raji	Function assay		4 h	IC50 = 0.069 μM	24900758
MM1S	Antiproliferative activity assay		72 h	IC50 = 0.0691 μM	29525435
BL21 (DE3)-codon plus-RIL	Fluorescence polarization assay		by fluorescence anisotropy assay	IC50 = 0.07 μM	28586718
22Rv1	Antiproliferative activity assay		96 h	IC50 = 0.071 μM	29758518
22Rv1	Antiproliferative activity assay		12 h	IC50 = 0.071 μM	29541371
BL21(DE3)-R3-pRARE2	Function assay		30 mins	IC50 = 0.077 μM	26731490
BL21(DE3)-R3-pRARE2	Function assay		30 mins	IC50 = 0.077 μM	28195723
BL21(DE3)-R3-pRARE2	Function assay		30 mins	IC50 = 0.077 μM	29776834
MV4-11	Cytotoxicity assay		24 h	GI50 = 0.08 μM	26191363
MV411	Antiproliferative activity assay		72 h	IC50 = 0.08 μM	28314513
TY82	Antiproliferative activity assay		72 h	IC50 = 0.0808 μM	29525435
HL60	Function assay		24 h	IC50 = 0.086 μM	28549889
697	Cytotoxicity assay		5 days	EC50 = 0.09 μM	29170024
Loucy	Cytotoxicity assay		5 days	EC50 = 0.09 μM	29170024
HT-29	Growth inhibition assay		72 h	IC50 = 0.104 μM	25559428
MM1S	Growth inhibition assay		72 h	IC50 = 0.109 μM	25559428
T cells	Function assay		24 h	IC50 = 0.11 μM	28314513
HL60	Antiproliferative activity assay		72 h	IC50 = 0.11 μM	26869194
BL21(DE3)	Function assay		2.5 h	IC50 = 0.12 μM	29541371
H1299	Function assay		24 h	EC50 = 0.153 μM	28949521
HD-MB03	Cytotoxicity assay		5 days	EC50 = 0.16 μM	29758518
LNCAP	Antiproliferative activity assay		96 h	IC50 = 0.16 μM	29758518
Hs578T	Antiproliferative activity assay		12 h	IC50 = 0.16 μM	29758518
MV4-11	Antiproliferative activity assay		12 h	IC50 = 0.16 μM	29170024
LNCAP	Antiproliferative activity assay		12 h	IC50 = 0.16 μM	29541371
C4-2B	Antiproliferative activity assay		96 h	IC50 = 0.19 μM	29758518
C4-2B	Antiproliferative activity assay		12 h	IC50 = 0.19 μM	29541371
Vero E6	Antiviral activity assay		48 h	IC50 = 0.19275 μM	32353859
MCF7	Antiproliferative activity assay		12 h	IC50 = 0.2 μM	29758518
MV4-11	Cytotoxicity assay		72 h	IC50 = 0.242 μM	23517011
MX1	Antiproliferative activity assay		72 h	EC50 = 0.254 μM	28949521
HT-29	Antiproliferative activity assay		72 h	IC50 = 0.28 μM	26731490
HFL1	Antiproliferative activity assay		12 h	IC50 = 0.29 μM	29758518
MDA-MB-231	Growth inhibition assay		3 days	GC50 = 0.3 μM	28549889
MV4-11	Antiproliferative activity assay		48 h	EC50 = 0.33113 μM	28595007
HL60	Antiproliferative activity assay		48 h	EC50 = 0.74131 μM	28595007
NCI-H1975	Antiproliferative activity assay		12 h	IC50 = 1.23 μM	29758518
SAE	Function assay		4 h	IC50 = 1.38 μM	29649741
SAE	Function assay		4 h	IC50 = 1.49 μM	29649741
SAE	Function assay		4 h	IC50 = 1.51 μM	29649741
U2OS	Antiproliferative activity assay		12 h	IC50 = 1.62 μM	29758518
SAE	Function assay		4 h	IC50 = 1.63 μM	29649741
A549	Antiproliferative activity assay		12 h	IC50 = 1.67 μM	29758518
MCF7	Growth inhibition assay		3 days	GC50 = 1.7 μM	28549889
DU145	Antiproliferative activity assay		96 h	IC50 = 2.52 μM	29758518
DU145	Antiproliferative activity assay		12 h	IC50 = 2.52 μM	29541371
T47D	Growth inhibition assay		3 days	GC50 = 2.8 μM	28549889
PC3	Antiproliferative activity assay		96 h	IC50 = 3.01 μM	29758518
PC3	Antiproliferative activity assay		12 h	IC50 = 3.01 μM	29541371
HeLa	Antiproliferative activity assay		12 h	IC50 = 3.76 μM	29758518
K562	Growth inhibition assay		3 days	GC50 = 3.8 μM	28549889
A2780	Growth inhibition assay		3 days	GC50 = 4 μM	28549889
HL60	Cytotoxicity assay		24 h	IC50 = 5.3 μM	27266999
MV4-11	Cytotoxicity assay		24 h	IC50 = 6.4 μM	27266999
K562	Antiproliferative activity assay		72 h	IC50 = 9.12 μM	28314513
OVCAR5	Growth inhibition assay		3 days	GC50 = 12 μM	28549889
Rosetta2 DE3	Function assay			Kd = 0.0062 μM	26080064
Rosetta2 DE3	Function assay			Kd = 0.0067 μM	26080064
Rosetta2 DE3	Function assay			Kd = 0.0117 μM	26080064
Rosetta2 DE3	Function assay			Kd = 0.0128 μM	26080064
Rosetta2 DE3	Function assay			Kd = 0.0136 μM	26080064
Rosetta2 DE3	Function assay			Kd = 0.0147 μM	26080064
BL21(DE3)	Function assay			Kd = 0.034 μM	26731490
Raji	Function assay			IC50 = 0.06 μM	26731490
MV4-11	Antiproliferative activity assay			IC50 = 0.072 μM	28195723
BL21(DE3)	Function assay			Kd = 0.092 μM	29541371
BL21(DE3)-R3-pRARE2	Function assay			Kd = 0.1 μM	28595007
LNCAP cells	Antiproliferative activity assay			IC50 = 0.1096 μM	29758518
BL21(DE3)	Function assay			IC50 = 0.12 μM	26731490
MV4-11	Antiproliferative activity assay			IC50 = 0.24 μM	27142751
K562	Antiproliferative activity assay			IC50 = 0.64 μM	27142751
点击查看更多细胞系数据

生物活性

产品描述

特性

(+)-JQ1比(-)-JQ1更有效。

靶点

BRD4 (2) ^[1] (Cell-free assay)	BRD4 (1) ^[1] (Cell-free assay)
33 nM	77 nM

体外研究(In Vitro)
体外研究活性	(+)-JQ1对映体直接结合到BET bromodomain结构域的Kac结合位点。(+)-JQ1(500 nM)与染色质竞争性结合到BRD4，导致NMC细胞分化和生长停滞。通过Ki67染色减少，证明了(+)-JQ1(500 nM)减弱NMC 797和Per403细胞系的快速增殖。(+)-JQ1(500 nM)作用于NMC 797细胞，有效降低BRD4靶基因的表达。(+)-JQ1作用于NMC 11060细胞，抑制细胞活力， IC50为4 nM。^[1](+)-JQ1作用于MM细胞系，强抑制MYC表达。(+)-JQ1抑制KMS-34和LR5增殖，IC50分别为 68 nM和98 nM。(+)-JQ1(500 nM)处理MM.1S细胞，导致S期细胞比例明显下降，随之细胞停滞在G0/G1期增多。(+)-JQ1(500 nM)通过β-半乳糖苷酶染色，导致明显的细胞衰老。(+)-JQ1(800 nM)处理CD138+病患衍生的MM样本，显著降低细胞活力。^[2] (+)-JQ1抑制LP-1细胞生长，GI50 为98 nM。(+)-JQ1(625 nM)导致LP-1细胞在G0/G1期的百分数增高。(+)-JQ1(500 nM)作用于LP-1细胞，抑制MYC, BRD4 和CDK9表达。^[3](+)-JQ1(1 μM)处理潜伏感染的Jurkat T细胞，激活HIV转录。(+)-JQ1(50 μM)作用于Jurkat和HeLa细胞，主要刺激Tat依赖性的HIV转录。(+)-JQ1(5 μM)作用于J-Lat A2细胞，诱导Brd4解离，从而使Tat招募SEC到HIV启动子上，诱导Pol II CTD磷酸化和病毒转录。^[4]
细胞实验	细胞系	MC 11060细胞
	浓度	~500 nM
	孵育时间	48小时
	方法	细胞按每孔500个接种在白色, 384孔微孔板，孔中含总体为50 μL的培养基。797, TT和TE10细胞生长在含1% Penicillin/Streptomycin 和 10% FBS的DMEM培养基上。Per403细胞生长在含1 % Penicillin/Streptomycin和20% FBS的DMEM 培养基上。病患衍生的NMC 11060细胞生长在含10% FBS 和1% Penicillin/Streptomycin的RPMI培养基上。通过自动化针转移机将(+)-JQ1置于微量检测板上。使细胞裂解，通过增殖试验测评孔中的总ATP含量。根据剂量，重复测量分析，通过逻辑回归（GraphPad Prism）计算IC50。
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	pDNA-PKcs / γH2AX / Ub-γH2AX / p-c-Jun S63 / Bax c-Myc p27		26119999
	Growth inhibition assay	Cell viability		23792448
	Immunofluorescence	GM130 MHC / EdU		29074567

体内研究(In Vivo)
体内研究活性	(+)-JQ1(50 mg/kg)处理携带NMC 797移植瘤的小鼠，抑制肿瘤生长。(+)-JQ1(50 mg/kg) 抹消掉携带NMC 797移植瘤的小鼠的NUT核斑点, 与竞争性结合到核染色质相一致。(+)-JQ1(50 mg/kg)处理NMC 797移植瘤，显著诱导（31级）角蛋白表达。(+)-JQ1(50 mg/kg)处理携带NMC移植瘤的小鼠模型，促进分化，肿瘤衰退，延长寿命。^[1](+)-JQ1(50 mg/kg)处理静脉注射MM.1S-luc+细胞，携带原位移植瘤的SCID米色小鼠，与对照组动物相比，显著延长小鼠的总生存期。^[2](+)-JQ1(50 mg/kg，腹腔注射)处理携带Raji移植瘤的小鼠，显著提高小鼠寿命。^[3]
动物实验	Animal Models	携带NMC 797移植瘤的小鼠
	Dosages	50 mg/kg
	Administration	腹腔注射

参考文献
[1] Filippakopoulos P, et al. Nature, 2010, 468(7327), 1067-1073. [2] Delmore JE, et al. Cell, 2011, 146(6), 904-917. [3] Mertz JA, et al. Proc Natl Acad Sci U S A, 2011, 108(40), 16669-16674. [4] Li Z, et al. Nucleic Acids Res, 2013, 41(1), 277-287. + 展开

参考文献

[4] Li Z, et al. Nucleic Acids Res, 2013, 41(1), 277-287.

+ 展开

化学信息&溶解度

分子量	456.99	分子式	C₂₃H₂₅ClN₄O₂S
CAS号	1268524-70-4	SDF	Download (+)-JQ1 SDF
Smiles	CC1=C(SC2=C1C(=NC(C3=NN=C(N32)C)CC(=O)OC(C)(C)C)C4=CC=C(C=C4)Cl)C
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 91 mg/mL ( (199.12 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 91 mg/mL (199.12 mM)

Water : Insoluble

DMSO : 91 mg/mL ( (199.12 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 91 mg/mL (199.12 mM)

Water : Insoluble

DMSO : 91 mg/mL ( (199.12 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Ethanol : 91 mg/mL (199.12 mM)

Water : Insoluble

摩尔浓度计算器

体内溶解度批次：现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂					动物体内配方计算器
体内溶解度批次：现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂	澄清溶液	5%DMSO 1 40%PEG 300 2 5%Tween80 3 50% ddH2O	5.0mg/ml (10.94mM)	以 1 mL 工作液为例，取 50 μL 100 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀使其澄清；向上述体系中加入50 μL Tween-80，混合均匀使其澄清；然后继续加入 500 μLddH2O定容至 1 mL。工作液请现配现用！	动物体内配方计算器
澄清溶液	5%DMSO 1 95% Corn oil	0.625mg/ml (1.37mM)	以 1 mL 工作液为例，取 50 μL12.5 mg/mL 的澄清 DMSO 储备液加到 950 μL玉米油中，混合均匀。工作液请现配现用！
澄清溶液	2% DMSO 1 30% PEG 300 2 5%Tween80 3 63%ddH2O	3.34mg/ml (7.31mM)	以 1 mL 工作液为例,取20 μL 167mg/ml的澄清DMSO储备液加到300 μL PEG300中,混合均匀使其澄清;向上述体系中加入50 μL Tween80,混合均匀使其澄清;然后继续加入630 μL ddH2O定容至1mL。工作液请现配现用!

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

技术支持

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操作手册

如果有其他问题，请给我们留言。

* 必填项

常见问题及建议解决方法

问题 1:
How can I reconstitute the compound for in vivo injection?

回答：
JQ1 does not dissolve in water/PBS. The vehicle we recommend is 2% DMSO+30% PEG 300+5% Tween 80+ddH2O. The compound can be dissolved in the vehicle at 5mg/ml and you can use it for IV injection.

C1=C0/X	C1:	LOG(C1):
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C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
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C8=C7/X	C8:	LOG(C8):